A Novel Series of DNA Triple Helix-Binding Ligands

We have examined the effect of a series of substituted imidazothioxanthones on the stability of an intermolecular DNA triple helix by DNase I footprinting. We find that several of these compounds promote the formation of a complex between T5C5and the target site A6G6·C6T6, suggesting that they bind...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 1996-07, Vol.224 (3), p.717-720
Main Authors: Fox, Keith R., Thurston, David E., Jenkins, Terence C., Varvaresou, Athanasia, Tsotinis, Andrew, Siatra-Papastaikoudi, Theodora
Format: Article
Language:English
Subjects:
Deoxyribonuclease I - metabolism
DNA - chemistry
DNA - drug effects
DNA Footprinting
Xanthenes - chemistry
Xanthenes - pharmacology
Xanthones
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Summary:We have examined the effect of a series of substituted imidazothioxanthones on the stability of an intermolecular DNA triple helix by DNase I footprinting. We find that several of these compounds promote the formation of a complex between T5C5and the target site A6G6·C6T6, suggesting that they bind specifically to triplex DNA. The only inactive derivative lacked a protonatable function in the side chain, suggesting that this is an essential feature for triplex stabilization. These compounds, which are amongst the first triplex-binding ligands which possess an uncharged chromophore, are selective for the T·AT rather than the C+·GC triplet.
ISSN:0006-291X
1090-2104
DOI:10.1006/bbrc.1996.1089